专利号:EP-2231627-B1 优先权日:2007-12-03 标题 :New process for the synthesis of moguisteine 发明人:VIGANO' ENRICO; ARRIGHI MASSIMILIANO; MOLTENI RENATO; LANFRANCONI SIMONA; LANDONIO ERNESTO 权利人:A M S A ANONIMA MATERIE SINT E AFFINI S P A 摘要:The invention relates to a process for the synthesis of moguisteine that is ethyl ester of (R,S)-3-[2-[(2-methoxyphenoxy)methyl]-1,3-thiazolidin-3-yl]-3-oxypropanoic acid which comprises the steps of forming a new cyclic intermediate of formula 2-[(2-methoxyphenoxy)methyl]-1,3-dioxolane (4), forming (R,S)-2-[(2-methoxyphenoxy)methyl]-1,3-thiazolidine (6) and reacting this latter with monoethylmalonic acid (7) or a salt thereof. The moguisteine of the invention is obtained in high yield and purity.
专利号:US-6096874-A 优先权日:1990-10-01 标 题:High affinity tamoxifen derivatives 发明人:WALLACE SIDNEY; YANG DAVID; DELPASSAND EBRAHIM; CHERIF ABDALLAH; QUADRI SYED M 权利人:UNIV TEXAS 摘要:The synthesis of tamoxifen derivatives, most particularly halo, halo alkyl, hydroxy, and amino tamoxifen derivatives is disclosed. The native tamoxifen molecule includes a substituted chemical group positioned on the aliphatic chain of the tamoxifen molecule. Particular tamoxifen derivatives of the invention include chloro, bromo, iodo, fluoro, amino and DTPA tamoxifen derivatives, and corresponding lower alkyl halogenated forms. The halogenated tamoxifen derivatives possess superior binding affinities for estrogen receptor rich tissues, such as uterine tissue and breast tissue, relative to unsubstituted native tamoxifen. Radiolabeled forms of the tamoxifen derivatives may be used as highly specific imaging agents for estrogen receptor rich tissues. The fluoro and bromo tamoxifen derivatives are particularly useful for imaging estrogen receptors by PET whereas the iodinated tamoxifens are particularly useful in imaging estrogen receptors by SPECT. Rapid and efficient methods of preparing the tamoxifen derivatives having high specific activity (>6 Ci/μmol) are also disclosed. Aliphatic chain substituted tamoxifen derivatives are shown to possess greater estrogen receptor binding affinity and more potent tumor cell inhibition than tamoxifen or tamoxifen derivatives substituted at other locations on the molecule (i.e., non-aliphatic chain substituted tamoxifen). The tanioxifen derivatives of the present invention may advantageously be used as anti-cancer therapeutic agents to halt estrogen-receptor positive tumors, such as those of breast and uterine tissue. The present invention also provides a hydrophilic DTPA-tamnoxifen analogue, and uses thereof in imaging estrogen receptor positive ER+ lesions.
专利号:US-7858821-B2 优先权日:2007-11-13 标题 :Intermediate compounds useful to prepare dolasetron 发明人:ANDRES JUAN ANTONIO PEREZ; BARJOAN PERE DALMASES; CLOTET JOAN HUGUET 权利人:INKE SA 摘要:The present invention relates to intermediates useful in the synthesis of Dolasetron and synthetic precursors thereof, as well as to processes for obtaining them. In addition, it refers to the hydrochloric salt of Dolasetron and polymorphic forms of Dolasetron and precursors thereof.
专利号:WO-2009071528-A2 优先权日:2007-12-03 标题 :New process for the synthesis of moguisteine
专利号:US-6586615-B1 优先权日:2001-01-10 标题:α-aminoboronic acids prepared by novel synthetic methods 发明人:KETTNER CHARLES A; JAGANNATHAN SHARADA; FORSYTH TIMOTHY PATRICK 权利人:BRISTOL MYERS SQUIBB CO 摘要:The present invention relates to a novel class of alpha-aminoboronic acids of Formula (V),which are useful as intermediates in synthetic processes for inhibitors of the serine proteases, leukocyte elastase, pancreatic elastase, cathepsin G, and chymotrypsin. More specifically, the alpha-aminoboronic acids are useful as intermediates for the synthesis of Hepatitis C Virus (HCV) protease inhibitors. This invention also generally relates to novel methods for the preparation of alpha-aminoboronic acids.
专利号:EP-1639121-A4 优先权日:2003-06-30 标题:SYNTHESIS OF BETA-L-2-DESOXYNUCLEOSIDES
[参考文献]: K Kamei, Et Al. New 5-Ht1A Receptor Agonists Possessing 1,4-Benzoxazepine Scaffold Exhibit Highly Potent Anti-Ischemic Effects. Bioorg Med Chem Lett. 2001 Feb 26;11(4):595-8.
合成参考文献
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